SHP2/HDAC-IN-1
SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.
For research use only. We do not sell to patients.
- CAS No.: 2831230-38-5
- Formula: C34H35Cl2N7O3
- Molecular Weight:660.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC1 25 nM (IC50) |
HDAC2 79 nM (IC50) |
HDAC3 233 nM (IC50) |
HDAC6 27 nM (IC50) |
SHP2 20.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
5.43 μM
Compound: 8t
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Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against mouse 4T1 cells assessed as cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
| ASPC1 | IC50 |
2.31 μM
Compound: 8t
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Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human ASPC1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
| BXPC-3 | IC50 |
1.65 μM
Compound: 8t
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Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
| KYSE-520 cell line | IC50 |
1.95 μM
Compound: 8t
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Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
| MV4-11 | IC50 |
0.07 μM
Compound: 8t
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
| SW1990 | IC50 |
3.92 μM
Compound: 8t
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Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36097406] |
SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells[1].
SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3[1].
SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Pancreatic carcinoma (BxPC-3, SW1990, and AsPC-1), acute monocytic leukemia (MV4-11)
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Concentration:0-10 μM approximately
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Incubation Time:72 h
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Result:Inhibited cell proliferation with IC50s range of 0.07 μM-3.92 μM.
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Cell Line:MV4-11 cells
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Concentration:0.25, 0.5, 1 μM
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Incubation Time:24 h
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Result:Increased the acetylation of α-tubulin and histone H3.
Inhibited the phosphorylation level of ERK.
SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 tumor-bearing xenograft mice[1]
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Dosage:40 mg/kg
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Administration:Oral adminstration (p.o.), every day for 20 consecutive days.
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Result:Delayed tumor progression with a tumor growth inhibition rate (TGI %) value of 64.0%, with no obvious signs of toxicity.
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Animal Model:4T1 murine breast cancer model[1]
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Dosage:40 mg/kg
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Administration:Oral adminstration (p.o.), every day for 12 consecutive days.
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Result:Significantly decreased tumor burden with a TGI value of 72%.
Increased the proportions of CD4+ T cells and CD8+ T cells in the spleen.
Enhanced the proportion of mDCs in lymph nodes.
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Animal Model:Male Sprague-Dawley (SD) rats (Pharmacokinetic assay)[1]
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Dosage:20 mg/kg p.o., 1 mg/kg i.v.
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Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
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Result:Pharmacokinetic profile of SHP2/HDAC-IN-1 (compound 8t).
dose (mg/kg) T1/2 (h) Cmax (ng/mL) Cl (mL/h/kg) F (%) 20 (p.o.) 5.32 1835 21.42 1 (i.v.) 6.15 3517 326
Chemical Information
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CAS No. 2831230-38-5
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Molecular Weight 660.59
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Formula C34H35Cl2N7O3
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SMILES
O=C(NCC1=CC=C(/C=C/C(NO)=O)C=C1)C2=CC=C(CNC3(C)CCN(C4=NC(N)=C(C5=C(Cl)C(Cl)=CC=C5)N=C4)CC3)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SHP2/HDAC-IN-1 Related Classifications
HY-151464 Related Classifications
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